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Astatine is an \u03b1-emitter (half-life=7.2 h) that can be produced by a 30-MeV cyclotron. This study evaluated the treatment effect of\n                      <jats:sup>211<\/jats:sup>\n                      At-labeled PSMA compounds in mouse xenograft models.\n                    <\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Methods<\/jats:title>\n                    <jats:p>\n                      Tumor xenograft models were established by subcutaneous transplantation of human prostate cancer cells (LNCaP) in NOD\/SCID mouse. [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA1, [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA5, or [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA6 was administered to LNCaP xenograft mice to evaluate biodistribution at 3 and 24 h. The treatment effect was evaluated by administering [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA1 (0.40 \u00b1 0.07 MBq), [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA5 (0.39 \u00b1 0.03 MBq), or saline. Histopathological evaluation was performed for the at-risk organs at 3 and 6 weeks after administration.\n                    <\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Results<\/jats:title>\n                    <jats:p>\n                      [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA5 resulted in higher tumor retention compared to [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA1 and [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA6 (30.6 \u00b1 17.8, 12.4 \u00b1 4.8, and 19.1 \u00b1 4.5 %ID\/g at 3 h versus 40.7 \u00b1 2.6, 8.7 \u00b1 3.5, and 18.1 \u00b1 2.2%ID\/g at 24 h, respectively), whereas kidney excretion was superior in [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA1 compared to [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA5 and [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA6. An excellent treatment effect on tumor growth was observed after [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA5 administration. [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA1 also showed a substantial treatment effect; however, the tumor size was relatively larger compared to that with [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA5. In the histopathological evaluation, regenerated tubules were detected in the kidneys at 3 and 6 weeks after the administration of [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA5.\n                    <\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Conclusion<\/jats:title>\n                    <jats:p>\n                      TAT using [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA5 resulted in excellent tumor growth suppression with minimal side effects in the normal organs. [\n                      <jats:sup>211<\/jats:sup>\n                      At]PSMA5 should be considered a new possible TAT for metastatic CRPC, and translational prospective trials are warranted.\n                    <\/jats:p>\n                  <\/jats:sec>","DOI":"10.1007\/s00259-022-06016-z","type":"journal-article","created":{"date-parts":[[2022,11,7]],"date-time":"2022-11-07T23:30:44Z","timestamp":1667863844000},"page":"849-858","update-policy":"https:\/\/doi.org\/10.1007\/springer_crossmark_policy","source":"Crossref","is-referenced-by-count":56,"title":["Targeted \u03b1-therapy using astatine (211At)-labeled PSMA1, 5, and 6: a preclinical evaluation as a novel compound"],"prefix":"10.1007","volume":"50","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-8658-2395","authenticated-orcid":false,"given":"Tadashi","family":"Watabe","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kazuko","family":"Kaneda-Nakashima","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yoshifumi","family":"Shirakami","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yuichiro","family":"Kadonaga","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kazuhiro","family":"Ooe","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yang","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hiromitsu","family":"Haba","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Atsushi","family":"Toyoshima","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jens","family":"Cardinale","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Frederik L.","family":"Giesel","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Noriyuki","family":"Tomiyama","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Koichi","family":"Fukase","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"297","published-online":{"date-parts":[[2022,11,8]]},"reference":[{"issue":"3","key":"6016_CR1","doi-asserted-by":"publisher","first-page":"209","DOI":"10.3322\/caac.21660","volume":"71","author":"H Sung","year":"2021","unstructured":"Sung H, Ferlay J, Siegel RL, Laversanne M, Soerjomataram I, Jemal A, et al. 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The protocol was approved by the Animal Care and Use Committee of the Osaka University Graduate School of Medicine (approval number: 30-103-011).","order":2,"name":"Ethics","group":{"name":"EthicsHeading","label":"Ethics approval"}},{"value":"Not applicable.","order":3,"name":"Ethics","group":{"name":"EthicsHeading","label":"Consent to participate"}},{"value":"Not applicable.","order":4,"name":"Ethics","group":{"name":"EthicsHeading","label":"Consent for publication"}},{"value":"The authors declare no potential conflicts of interest relevant to this study. FLG is advisor at ABX, Telix, SOFIE Biosciences and Alpha Fusion. FLG and JC have a patent application on PSMA-1007. TW, KK, YS, YK, AT, and KF have a patent application on [<sup>211<\/sup>At]-labeled PSMA.","order":5,"name":"Ethics","group":{"name":"EthicsHeading","label":"Conflict of interest"}}]}}